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WO2004021969A3 - Inhibiteurs de la transcriptase inverse non nucleosidiques - Google Patents

Inhibiteurs de la transcriptase inverse non nucleosidiques Download PDF

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Publication number
WO2004021969A3
WO2004021969A3 PCT/EP2003/009872 EP0309872W WO2004021969A3 WO 2004021969 A3 WO2004021969 A3 WO 2004021969A3 EP 0309872 W EP0309872 W EP 0309872W WO 2004021969 A3 WO2004021969 A3 WO 2004021969A3
Authority
WO
WIPO (PCT)
Prior art keywords
independently
alkyl
reverse transcriptase
transcriptase inhibitors
nucleoside reverse
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2003/009872
Other languages
English (en)
Other versions
WO2004021969A2 (fr
Inventor
Dmitry Antonov
Christian Sund
Stefan Lindstroem
Christer Sahlberg
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Medivir AB
Original Assignee
Medivir AB
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Medivir AB filed Critical Medivir AB
Priority to CA002501924A priority Critical patent/CA2501924A1/fr
Priority to JP2004533489A priority patent/JP2005538155A/ja
Priority to AU2003260492A priority patent/AU2003260492B2/en
Priority to EP03793809A priority patent/EP1534276B1/fr
Priority to MXPA05002545A priority patent/MXPA05002545A/es
Priority to US10/526,598 priority patent/US7517992B2/en
Priority to DE60324568T priority patent/DE60324568D1/de
Publication of WO2004021969A2 publication Critical patent/WO2004021969A2/fr
Publication of WO2004021969A3 publication Critical patent/WO2004021969A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/65—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/93—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/94—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/78—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/04—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D335/06—Benzothiopyrans; Hydrogenated benzothiopyrans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • AIDS & HIV (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention a trait à un composé de formule (Y), dans laquelle : R1 est O, S ; R2 est un hétérocycle azoté ; R3 est H, alkyle en C1-C3 ; X est -(CR8R8')n-D-(CR8R8')m-; D est une liaison, -NR9-, -O-, -S-, -S(=O)- ou -S(=O)2-; R8 et R8' avec leur atome de carbone adjacent est -C(=O) ; R9 est indépendamment H, alkyle en C1-C3 ; E est -CH2-, -CHOH-, -C(=O)-, -NR9-, -O-, -S-, -S(=O)2-; n et m sont indépendamment 0,1 ou 2 ; p et q sont indépendamment 0,1 ou 2, où p+q ≤ 2 ; R10 est un système carbocyclique ou hétérocyclique éventuellement substitué ; R11 est indépendamment H, alkyle en C1-C3 alkyle en C1-C3 substitué par halo, hydroxy. Ledit composé est utile en tant qu'agent antiviral du VIH.
PCT/EP2003/009872 2002-09-05 2003-09-05 Inhibiteurs de la transcriptase inverse non nucleosidiques Ceased WO2004021969A2 (fr)

Priority Applications (7)

Application Number Priority Date Filing Date Title
CA002501924A CA2501924A1 (fr) 2002-09-05 2003-09-05 Inhibiteurs de la transcriptase inverse non nucleosidiques
JP2004533489A JP2005538155A (ja) 2002-09-05 2003-09-05 非ヌクレオシド逆転写酵素インヒビター
AU2003260492A AU2003260492B2 (en) 2002-09-05 2003-09-05 Non-nucleoside reverse transcriptase inhibitors
EP03793809A EP1534276B1 (fr) 2002-09-05 2003-09-05 Inhibiteurs de la transcriptase inverse non nucleosidiques
MXPA05002545A MXPA05002545A (es) 2002-09-05 2003-09-05 Inhibidores de transcriptasa inversa sin nucleosidos.
US10/526,598 US7517992B2 (en) 2002-09-05 2003-09-05 Non-nucleoside reverse transcriptase inhibitors
DE60324568T DE60324568D1 (en) 2002-09-05 2003-09-05 Nicht-nucleoside revers-transcriptase inhibitoren

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02019997.2 2002-09-05
EP02019997 2002-09-05

Publications (2)

Publication Number Publication Date
WO2004021969A2 WO2004021969A2 (fr) 2004-03-18
WO2004021969A3 true WO2004021969A3 (fr) 2004-08-05

Family

ID=31970278

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/009872 Ceased WO2004021969A2 (fr) 2002-09-05 2003-09-05 Inhibiteurs de la transcriptase inverse non nucleosidiques

Country Status (12)

Country Link
US (1) US7517992B2 (fr)
EP (1) EP1534276B1 (fr)
JP (1) JP2005538155A (fr)
KR (1) KR20050033663A (fr)
CN (1) CN1694700A (fr)
AT (1) ATE413174T1 (fr)
AU (1) AU2003260492B2 (fr)
CA (1) CA2501924A1 (fr)
DE (1) DE60324568D1 (fr)
MX (1) MXPA05002545A (fr)
WO (1) WO2004021969A2 (fr)
ZA (1) ZA200501805B (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7915295B2 (en) 2004-01-08 2011-03-29 Medivir Ab Non-nucleotide reverse transcriptase inhibitors
WO2007136573A2 (fr) 2006-05-15 2007-11-29 Merck & Co., Inc. Composés bicycliques antidiabétiques
AU2008319418B2 (en) * 2007-10-29 2013-08-15 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
ES2686821T3 (es) 2013-06-28 2018-10-22 Beigene, Ltd. Compuestos tricíclicos fusionados de urea como inhibidores de Raf quinasa y/o dímero de Raf quinasa
EP3013797B1 (fr) * 2013-06-28 2018-01-03 BeiGene, Ltd. Composés amides tricycliques condensés comme inhibiteurs de kinases multiples
GB201522179D0 (en) * 2015-12-16 2016-01-27 Autifony Therapeutics Ltd Novel compounds
CN110551063A (zh) * 2019-10-17 2019-12-10 山东邹平大展新材料有限公司 一种合成5-(n-boc-哌嗪-1-基)吡啶-2-胺的方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000047561A1 (fr) * 1999-02-12 2000-08-17 Medivir Ab Inhibiteurs non nucleosidiques de la transcriptase inverse
WO2002070516A2 (fr) * 2001-03-05 2002-09-12 Medivir Ab Inhibiteurs non-nucleosidiques de la transcriptase inverse
WO2003020705A1 (fr) * 2001-08-28 2003-03-13 Medivir Ab Derives d'uree et de thio-uree utilise comme inhibiteurs non nucleosidiques de la transcriptase inverse

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7915295B2 (en) * 2004-01-08 2011-03-29 Medivir Ab Non-nucleotide reverse transcriptase inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000047561A1 (fr) * 1999-02-12 2000-08-17 Medivir Ab Inhibiteurs non nucleosidiques de la transcriptase inverse
WO2002070516A2 (fr) * 2001-03-05 2002-09-12 Medivir Ab Inhibiteurs non-nucleosidiques de la transcriptase inverse
WO2003020705A1 (fr) * 2001-08-28 2003-03-13 Medivir Ab Derives d'uree et de thio-uree utilise comme inhibiteurs non nucleosidiques de la transcriptase inverse

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
HOEGBERG M ET AL: "Urea-PETT Compounds as a New Class of HIV-1 Reverse Transcriptase Inhibitors. 3. Synthesis and Further Structure-Activity Relationship Studies of PETT Analogues", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 42, no. 20, 1999, pages 4150 - 4160, XP002210257, ISSN: 0022-2623 *

Also Published As

Publication number Publication date
DE60324568D1 (en) 2008-12-18
ATE413174T1 (de) 2008-11-15
US20060167055A1 (en) 2006-07-27
MXPA05002545A (es) 2005-09-30
EP1534276A2 (fr) 2005-06-01
US7517992B2 (en) 2009-04-14
WO2004021969A2 (fr) 2004-03-18
ZA200501805B (en) 2005-09-08
CN1694700A (zh) 2005-11-09
CA2501924A1 (fr) 2004-03-18
AU2003260492B2 (en) 2007-03-01
JP2005538155A (ja) 2005-12-15
EP1534276B1 (fr) 2008-11-05
AU2003260492A1 (en) 2004-03-29
KR20050033663A (ko) 2005-04-12

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